ABSTRACT The objective of this study was to compare two alkaloids (antioquine and tetrandrine) with verapamil; knowing that the smooth muscle respond to KCl and relationships with calcium. The effects of antioquine and tetrandrine, was studied in adults Wistar rat with modified methods used in the determination of aorta contractility and compared with verapamil effect in the same assays. The analysis of the effect of a drug or extract on aortic reactivity included maximal relaxation or maximal contraction (Cmax) (Phase 1). In our results, verapamil induced a blockade of 98.7 ± 0.7% (n = 6) in presence of endothelium and 97.9 ± 4.3% in ausence of endothelium, both in phase 1 and in phase 2 of 47.4 ± 4.1% (n = 6) in aortas in the presence of endothelium and 61.8 ± 1.1% in ausence of endothelium; Tetrandrine assays showed a phase 1 blocking effect of 63.4 ± 5.5 and 47.7 ± 2.9% (with and without endothelium, respectively) and phase 2 of 43.5 ± 6.2 and 28.5 ± 5.7%, (with and without endothelium, respectively). Antioquine presents in phase 1 and phase 2, a blockade that is not significant from the point of view of calcium antagonism. We can conclude that tetrandrine block the movement of calcium from both intracellular and extracellular deposits, with the greatest effect when aortas are in the presence of endothelium.

A variety of 6-bromine-containing 7-anilino-1-arylisoquinolinequinones 2a-g were synthesized to evaluate their half-wave potentials and in vitro antiproliferative activity on gastric and leukemia cancer cell lines. The new compounds displayed significant IC50 values in the range: 1.31 to 11.04 μM. The structure activity relationship analysis of the new series suggest that the antiproliferative activity is dependent, in part, on the push-pull electronic effects of the nitrogen and bromine substituents inserted into the redox fragment of the 1-arylisoquinolinequinone scaffold. Linear regression analysis provided satisfactory relationships between the log IC50 and ClogP values for the AGS gastric cancer cell line.

Solar photoacylation of 1,4-naphthoquinone with 4-methoxybenzaldehyde to give (1,4-dihydroxynaphthalen-2-yl)(4'-methoxyphenyl) methanone is one representative example of a general procedure to prepare highly functionalized 1,4-dihydroxynaphthalen-2-yl)(phenyl) methanone derivatives. The structure of the title compound was confirmed by x-ray diffraction analysis of a suitable single crystal.

A simple and rapid analytical method is developed and validated for the determination of antiepileptic and antipsychotic drugs in human whole blood using a solid-phase extraction and quantification by gas chromatography-mass spectrometry (GC/MS). Prazepam was used as internal standard (IS). The specificity, linearity, intra- and inter-assay precision and accuracy, and extraction recovery were fully evaluated. The limits of detection and quantification were in the range of 0.52 - 0.98 μg/mL and 1.56 - 2.97 μg/mL for antiepileptic drugs (pentobarbital, phenobarbital and carbamazepine) and 1.31 - 2.94 ng/mL and 3.98 - 8.89 ng/mL for antipsychotic drugs (chlorpromazine and thioridazine), respectively. The relative standard deviation (RSD) was less than 7.07%, while the intra-day accuracy was < 3.21% and the inter-day was < 8.80%, referred to RSD. The developed methodology was applied in forensic cases of death caused by phenothiazines in the North of Chile during 2010-2012.

The consumption of antidepressant drugs has increased in these last years, leading to severe and lethal poisonings. In this work, analytical tools, namely GC/MSD and GC/NPD µECD, were used to identify and quantify several antidepressant drugs including amitriptyline, imipramine, sertraline, fluoxetine, and citalopram in forensic cases in the North of Chile during 2008-2011. Drugs were analyzed in biological arrays like blood. A solid phase extraction by Bond Elut Certify columns was applied in all these processes. Fluoxetine and sertraline were derivatized with pentafluoropropionic anhydride. Prazepam was used as internal standard (IS). The limit of detection (LOD) in blood were 0.5 - 20.07 ng/mL. The average extraction rate was 89.39% in blood. The relative standard deviation (RSD) was less than 3.6%, while the intra-day accuracy was < 5.5% and the inter-day was < 2.4%, referred to RSD. The procedures we have developed allow the quantification of drugs even at low therapeutic doses, a very important issue taking into account the nature of the analyzed arrays.

The present paper describes a method for the simultaneous determination of cocaine and benzoylecgonine in human whole blood. The drugs were extracted with phosphate buffer at pH 6, followed by solid-phase extraction and quantification by GC/MS with electron impact ionization using helium as carrier gas. Quantification was performed using cocaine-d3 as internal standard in selected ion monitoring mode. The method is very simple, rapid and sensitive. The specificity, linearity, intra- and inter-assay precision and accuracy, and extraction recovery were fully evaluated. The limits of detection were 3.6 ng/mL for cocaine and 6.8 ng/mL for benzoylecgonine. The method was applied to blood samples removed at autopsy from body packers and stuffers cases in the I - IV and XV regions of Chile during 2008-2010.

An essential oil from Senecio atacamensis Phil. (Asteraceae) was obtained by hydrodistillation of its aerial parts (leaves and stems) and its composition was determined by GC and GC/MS analysis. The identification by GC of the essential oil components, in both leaves and stems respectively, showed α-terpinene (36.05% and 20.57%); α-phellandrene (27.79% and 25.37%), and p-cymene (11.85% and 22.55%) as the most abundant monoterpenes. Furthermore, the oil was tested for its antimicrobial activity using paper disc diffusion and the dilution broth method, exhibiting moderate inhibition of human pathogenic bacteria.

A rapid, selective, sensitive, and specific method is presented to simultaneously quantify morphine, 6-monoacetylmorphine (6-MAM), codeine, heroin, fentanyl, and methadone in human whole blood and plasma. The drugs were extracted with phosphate buffer at pH 6, followed by solid-phase extraction (SPE) and quantification by GC/MS with electron impact ionization using helium as carrier gas. Quantification was performed based on nalorphine as internal standard (IS). The specificity, linearity, intra- and inter-assay precision and accuracy, and extraction recovery were fully evaluated. The limits of detection (LODs) were 0.40 - 7.63 ng/mL for whole blood and 0.80 - 32.00 ng/mL for plasma. The method is fast, simple, and accurate, with the sensitivity and specificity required in forensic and clinical toxicology.

Four benzodiazepines flunitrazepam, nitrazepam, clonazepam, and alprazolam, have been analyzed from biological matrices by dual column gas chromatography using a nitrogen-phosphorus detector (NPD) and a micro-electron capture detector (m-ECD). The recoveries of the four benzodiazepines spiked into human whole blood and plasma were 88.8 - 97.9 and 90.7 - 97.5%, respectively. The regression equations for the four benzodiazepines showed excellent linearity. The detection limits (LODs) were 0.14 - 0.95 ng/mL for whole blood and 0.13 - 0.93 ng/mL for plasma. The method is simple and sensitive for the determination of benzodiazepines in human whole blood and plasma, and may be useful in forensic science practice.

The composition of the essential oil from Pantana cámara L. (Verbenaceae) obtained by hydrodistillation of the aerial parts was examined by GC, GC/ MS, and 13C-NMR. The GC analysis showed that carvone is the most abundant monoterpene 75.9%, together with limonene 16.9%, accounting for 92.8% of the oil. The major components were also tested by "C-NMR analysis of the essential oil. The L. cámara oil was assayed against several microorganisms, showing moderate antibacterial activity against the human pathogen Staphylococcus aureus (MIC 200 µg/ml). High antioxidant activity evaluated by the Trolox equivalent antioxidant capacity assay (TEAC) was found (29.0 mmol Trolox/kg) and relative low anti-inflammatory activity due to its weak ability for inhibiting lipoxygenase (IC50 = 81.5 µg/ml).

The preparation of oxygenated derivatives of ambrox and isoambrox is described. The compounds 8á-hydroxy-isoambrox, 7β-hydroxy-isoambrox, 8á-hydroxy-ambrox, 7β-hydroxy-ambrox, 7-oxo-isoambrox and 7-oxo-ambrox have been synthesized from (-)-drimenol, readily available from the bark of Drimys winteri. The structures of the products were determined mainly by spectroscopic methods